Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors

Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evalua...

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Detalles Bibliográficos
Autores: Mosolygó, Tímea, Kincses, Annamária, Csonka, Andrea, Tönki, Ádám Szabó, Witek, Karolina, Sanmartín, Carmen, Marć, Małgorzata Anna, Handzlik, Jadwiga, Kieć-Kononowicz, Katarzyna, Domínguez-Álvarez, Enrique, Spengler, Gabriella
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/180727
Acceso en línea:http://hdl.handle.net/10261/180727
Access Level:acceso abierto
Palabra clave:Selenocompounds
Selenoesters
AcrAB-TolC efflux pump
Chlamydia trachomatis D
Escherichia coli K-12 AG100
Staphylococcus aureus
Descripción
Sumario:Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evaluated. The effects of eleven selenocompounds on bacterial growth were evaluated in <i>Staphylococcus aureus</i>, methicillin resistant <i>S. aureus</i> (MRSA), <i>Enterococcus faecalis, Escherichia coli</i>, and <i>Chlamydia trachomatis</i> D. The combination effect of compounds with antibiotics was examined by the minimum inhibitory concentration reduction assay. Their efflux pump (EP) inhibitory properties were assessed using real-time fluorimetry. Relative expressions of EP and quorum-sensing genes were studied by quantitative PCR. Results showed that a methylketone selenoester had remarkable antibacterial activity against Gram-positive bacteria and potentiated the activity of oxacillin in MRSA. Most of the selenocompounds showed significant anti-chlamydial effects. The selenoanhydride and the diselenodiester were active inhibitors of the AcrAB-TolC system. Based on these results it can be concluded that this group of selenocompounds can be attractive potential antibacterials and EP inhibitors. The discovery of new derivatives with a significant antibacterial activity as novel selenocompounds, is of high impact in the fight against resistant pathogens.